Chemical studies on brassinosteroids and jasmonic acid biosynthesis inhibitors(The JSCRP Award,The Society Awards Lecture)

Abstract

Plants responses to internal signals and environmental stimuli are regulated by a complex mechanism of signal transduction networks. Plant hormones are important signal mediators that play key roles in signaling. Brassinosteroids (BRs) and jasmonic acid (JA) are plant hormones involved in plant development and defense responses to environmental stress. To explore the biological functions of their biosynthetic pathways, we conducted a systematic search for specific inhibitors of BRs biosynthesis and JA biosynthesis. The BRs biosynthesis inhibitors were developed based on the molecular scaffold of P450 inhibitors. Structure-activity relationship studies created YCZ-18, which is the most potent BRs biosynthesis inhibitor found to date. Development of the JA biosynthesis inhibitors was conducted based on the design of inhibitors targeting allene oxide synthase (AOS, CYP74A), a key enzyme of JA biosynthesis. This strategy led to the discovery of JM-8686, the first synthetic inhibitor of JA biosynthesis.